Tetrodotoxin (TTX) as a Therapeutic Agent for Pain
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AuthorNieto, Francisco Rafael; Cobos, Enrique José; Tejada, Miguel Ángel; Sánchez Fernández, Cristina; González Cano, Rafael; Cendán, Cruz Miguel
TetrodotoxinTTXTTX-sensitive voltage-gated sodium channelsPainNeuropathic pain
Nieto, F. R., Cobos, E. J., Tejada, M. Á., Sánchez-Fernández, C., González-Cano, R., & Cendán, C. M. (2012). Tetrodotoxin (TTX) as a therapeutic agent for pain. Marine Drugs, 10(2), 281-305. [DOI:10.3390/md10020281]
SponsorshipNational Health and Medical Research Council of Australia German Research Foundation (DFG); Spanish Government; University of Granada GREIB (CEB-005); Junta de Andalucía CTS 109
Tetrodotoxin (TTX) is a potent neurotoxin that blocks voltage-gated sodium channels (VGSCs). VGSCs play a critical role in neuronal function under both physiological and pathological conditions. TTX has been extensively used to functionally characterize VGSCs, which can be classified as TTX-sensitive or TTX-resistant channels according to their sensitivity to this toxin. Alterations in the expression and/or function of some specific TTX-sensitive VGSCs have been implicated in a number of chronic pain conditions. The administration of TTX at doses below those that interfere with the generation and conduction of action potentials in normal (non-injured) nerves has been used in humans and experimental animals under different pain conditions. These data indicate a role for TTX as a potential therapeutic agent for pain. This review focuses on the preclinical and clinical evidence supporting a potential analgesic role for TTX. In addition, the contribution of specific TTX-sensitive VGSCs to pain is reviewed.